title: Enhancing cell nucleus accumulation and DNA cleavage activity of anti-cancer drug via graphene quantum dots.
abstract: Graphene quantum dots (GQDs) maintain the intrinsic layered structural motif of graphene but with smaller lateral size and abundant periphery carboxylic groups, and are more compatible with biological system, thus are promising nanomaterials for therapeutic applications. Here we show that GQDs have a superb ability in drug delivery and anti-cancer activity boost without any pre-modification due to their unique structural properties. They could efficiently deliver doxorubicin (DOX) to the nucleus through DOX/GQD conjugates, because the conjugates assume different cellular and nuclear internalization pathways comparing to free DOX. Also, the conjugates could enhance DNA cleavage activity of DOX markedly. This enhancement combining with efficient nuclear delivery improved cytotoxicity of DOX dramatically. Furthermore, the DOX/GQD conjugates could also increase the nuclear uptake and cytotoxicity of DOX to drug-resistant cancer cells indicating that the conjugates may be capable to increase chemotherapy efficacy of anti-cancer drugs that are suboptimal due to the drug resistance.
authors.affiliation: 1] State Key Laboratory of Bioreactor Engineering, Shanghai Key Laboratory of New Drug Design, School of Pharmacy, East China University of Science and Technology, Shanghai, 200237. P. R. China [2].
authors.forename: Chong
authors.initials: C
authors.lastname: Wang
authors.forename: Congyu
authors.initials: C
authors.lastname: Wu
authors.forename: Xuejiao
authors.initials: X
authors.lastname: Zhou
authors.forename: Ting
authors.initials: T
authors.lastname: Han
authors.forename: Xiaozhen
authors.initials: X
authors.lastname: Xin
authors.forename: Jiaying
authors.initials: J
authors.lastname: Wu
authors.forename: Jingyan
authors.initials: J
authors.lastname: Zhang
authors.forename: Shouwu
authors.initials: S
authors.lastname: Guo
mesh_terms: D000970:Antineoplastic Agents / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism* / Q000633:toxicity; D001692:Biological Transport; D045744:Cell Line, Tumor; D002467:Cell Nucleus / Q000378:metabolism*; D053837:DNA Cleavage / Q000187:drug effects*; D004317:Doxorubicin / Q000008:administration & dosage / Q000737:chemistry / Q000378:metabolism / Q000633:toxicity; D006108:Graphite / Q000737:chemistry; D006801:Humans; D042541:Intracellular Space / Q000378:metabolism; D008954:Models, Biological; D045663:Quantum Dots / Q000737:chemistry
chemical_list: D000970:Antineoplastic Agents; D006108:Graphite; D004317:Doxorubicin